Effect of Fluid Paraffin on the Formulation Properties of Pressure Sensitive Adhesive Formulations Containing Diclofenac Sodium

IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY AAPS PharmSciTech Pub Date : 2024-10-15 DOI:10.1208/s12249-024-02959-8

Kaede Osanai, Shunsuke Aoki, Chihiro Otsuka, Hirotaka Watanabe, Haruhiko Hikichi, Takayuki Terukina, Hiromu Kondo

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Abstract

Understanding the relationship between the release characteristics of the active ingredient in the tape formulation and the pharmaceutical characteristics of the adhesive layer can optimize therapeutic efficacy and improve patient adherence. This study aimed to clarify the effect of liquid paraffine (LP)/styrene–isoprene-styrene (SIS) triblock copolymer ratio on pressure-sensitive adhesive (PSA) formulation properties, such as adhesive properties and drug release, with a certain amount of diclofenac sodium (DFS) and tackifier. The effects of changes in PSA composition in DFS-containing tape formulations on adhesive and drug release properties were evaluated. The viscoelasticity results showed rigid gel-like behavior at low angular frequencies regardless of the LP/SIS ratio, and deformable gel-like behavior at high angular frequencies, with a maximum plasticizing effect of LP up to an LP/SIS ratio of 3.7. The peel adhesion test results showed that peel adhesion was not affected, but indicated a decreasing trend by increasing the LP/SIS ratio in the presence of DFS. Drug release test results showed that DFS release increased up to 24 h for LP/SIS ratios of up to 3.7, but decreased when the LP/SIS ratio was 6. The results of the drug permeation tests were similar to those of the drug release tests. In conclusion, it is possible to change the drug release properties by changing the amount of LP in the tape formulation; however, no definitive correlation was found between the adhesive and drug release properties.

Graphical Abstract

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液体石蜡对含双氯芬酸钠的压敏胶配方性能的影响

了解胶带配方中活性成分的释放特性与粘合剂层的药物特性之间的关系可以优化疗效并提高患者的依从性。本研究旨在阐明液态石蜡（LP）/苯乙烯-异戊二烯-苯乙烯（SIS）三嵌段共聚物配比对含有一定量双氯芬酸钠（DFS）和增粘剂的压敏胶（PSA）配方性能（如粘合性能和药物释放）的影响。评估了含 DFS 胶带配方中 PSA 成分的变化对粘合性能和药物释放性能的影响。粘弹性结果表明，无论 LP/SIS 比为多少，在低角频率下都表现为刚性凝胶状，而在高角频率下则表现为可变形凝胶状，LP 的最大塑化效果可达 LP/SIS 比 3.7。剥离粘附力测试结果表明，剥离粘附力未受影响，但在有 DFS 的情况下，随着 LP/SIS 比的增加，剥离粘附力呈下降趋势。药物释放测试结果表明，当 LP/SIS 比率为 3.7 时，DFS 的释放时间最长可达 24 小时，但当 LP/SIS 比率为 6 时，DFS 的释放时间则有所减少。总之，可以通过改变胶带配方中的 LP 含量来改变药物释放性能；但在粘合剂和药物释放性能之间没有发现明确的相关性。

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.